Schedule H

Intravenous, Subcutaneous, Intradermal, Topical, Mucosal, Epidural, Spinal

• Injection: 1% (10 mg/mL), 2% (20 mg/mL) in 2 mL, 5 mL, 10 mL, 30 mL vials/ampoules

• Injection with adrenaline: 2% Lidocaine + Adrenaline 1:200,000

• Topical gel: 2%, 4%

• Ointment: 5%

• Spray: 10% (100 mg/mL)

• Jelly (urogenital): 2%

• Transdermal patch: 5% (limited availability)

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Local and Regional Anaesthesia

(Infiltration, peripheral nerve block, epidural, spinal)

Infiltration Anaesthesia:

Parameter Without Adrenaline With Adrenaline (1:200,000)

Starting dose 1–2% solution; calculate based on weight 1–2% solution; calculate based on weight

Titration Not applicable — single procedure dose Not applicable

Usual maintenance dose Not applicable Not applicable

Maximum dose 4.5 mg/kg (absolute max 300 mg) 7 mg/kg (absolute max 500 mg)

Peripheral Nerve Block:

Parameter Details

Starting dose 1–2% solution; dose calculated per weight

Titration Not applicable

Usual maintenance dose Not applicable

Maximum dose 4.5 mg/kg without adrenaline; 7 mg/kg with adrenaline

Epidural Anaesthesia:

Parameter Details

Starting dose 1.5–2% preservative-free solution

Titration Titrate to desired sensory level

Usual maintenance dose Bolus or continuous infusion per protocol

Maximum dose As per body weight limits; specialist supervision mandatory

Spinal Anaesthesia:

Parameter Details

Starting dose 5% hyperbaric solution; 50–100 mg single injection

Titration Not applicable — single-shot technique

Usual maintenance dose Not applicable

Maximum dose 100 mg per procedure

Clinical Notes:

• Use preservative-free formulations for spinal, epidural, and intrathecal routes

• Adrenaline-containing formulations contraindicated for spinal/IV use and end-artery regions

• Duration of action varies by site, concentration, and vasoconstrictor use

1. Ventricular Arrhythmias — Acute Management

(Ventricular tachycardia, ventricular fibrillation — particularly post-MI or refractory to defibrillation)

IV Administration (ICU/CCU/monitored settings only):

Parameter Details

Starting dose 1–1.5 mg/kg IV bolus over 2–3 minutes

Titration Repeat bolus 0.5–0.75 mg/kg every 5–10 minutes if arrhythmia persists

Usual maintenance dose Continuous IV infusion 1–4 mg/min (20–50 mcg/kg/min)

Maximum dose Total bolus: 3 mg/kg; Infusion: 4 mg/min; Total 24-hour dose: ≤300 mg

Clinical Notes:

• Continuous ECG monitoring mandatory

• Reduce maintenance infusion dose by 50% in hepatic impairment and elderly

• NOT first-line for VT/VF — amiodarone generally preferred per current ACLS protocols

• Avoid prolonged infusion (>24 hours) without specialist guidance

1. Topical/Mucosal Anaesthesia

(Minor procedures, catheterisation, endoscopy, wound care)

Gel/Ointment (2–5%):

Parameter Details

Starting dose Apply thin layer to affected area

Titration Not applicable

Usual maintenance dose 2–3 applications daily as needed

Maximum dose Limit total dose to 4.5 mg/kg; avoid large surface areas

Spray (10%):

Parameter Details

Starting dose 1–2 sprays (10–20 mg) to target area

Titration Not applicable

Usual maintenance dose Single application per procedure

Maximum dose 3–5 sprays (30–50 mg) per session

Jelly (2% — Urogenital):

Parameter Details

Starting dose 6–10 mL instilled into urethra (male) or 3–5 mL (female)

PAEDIATRIC DOSING (Specialist Only)

Primary Indications

1. Local and Regional Anaesthesia

Age/Weight Formulation Starting Dose Maximum Dose

All ages 0.5–1% solution (infiltration) 3–5 mg/kg 4.5 mg/kg without adrenaline; 7 mg/kg with adrenaline

Neonates (<1 month) Preservative-free only 3 mg/kg 4 mg/kg (lower threshold)

Monitoring:

• CNS signs of toxicity (irritability, drowsiness, seizures)

• Cardiovascular status

• Calculate dose carefully based on actual body weight

Clinical Notes:

• Use preservative-free formulations in neonates and infants

• Avoid adrenaline-containing formulations in neonates due to immature vasoregulation

• Large surface area topical application in infants increases systemic absorption risk

1. Ventricular Arrhythmias — Life-Threatening (PICU/NICU Only)

Parameter Details

Starting dose 1 mg/kg IV bolus over 2–3 minutes (maximum 50 mg)

Titration May repeat 0.5 mg/kg bolus if arrhythmia persists

Usual maintenance dose 20–50 mcg/kg/min continuous IV infusion

Maximum dose Total bolus 3 mg/kg; infusion rate 50 mcg/kg/min

Monitoring:

• Continuous ECG monitoring mandatory

• Blood pressure

• Serum lidocaine levels if infusion >24 hours or hepatic impairment

Secondary Indications — Paediatric (Off-label)

Indication Age Dose Remarks

Topical analgesia for minor procedures — OFF-LABEL ≥3 months 2% gel; thin layer to local area; max 3 applications/day Specialist supervision; avoid large surface areas

⚠️ Not recommended below 3 months of age except under specialist supervision (Anaesthesiology/NICU/PICU) with documented justification. Systemic absorption risk significantly higher in neonates and young infants.

No dose adjustment routinely required — lidocaine is primarily hepatically metabolised.

Caution: Active metabolites (monoethylglycinexylidide [MEGX], glycinexylidide [GX]) may accumulate with prolonged IV infusion (>24 hours) in severe renal impairment — monitor for neurotoxicity.

Note: Lidocaine undergoes extensive hepatic metabolism via CYP1A2 and CYP3A4 — half-life significantly prolonged in hepatic dysfunction.

• Known hypersensitivity to lidocaine or other amide-type local anaesthetics (bupivacaine, ropivacaine, mepivacaine)

• Adams-Stokes syndrome (complete heart block with syncope)

• Wolff-Parkinson-White syndrome (for IV antiarrhythmic use)

• Second-degree or third-degree AV block without functioning pacemaker (for IV use)

• Severe sinoatrial block without pacemaker

• Injection into infected or acutely inflamed tissue (for regional blocks)

• Hypovolaemic shock (for IV antiarrhythmic use)

• Severe hepatic failure (for continuous IV infusion)

• Intravenous regional anaesthesia (Bier block) in patients with severe peripheral vascular disease

• Elderly patients — reduced hepatic clearance; increased sensitivity to CNS effects

• Malnourished or debilitated patients — lower plasma protein binding; increased free drug

• Cardiac dysfunction — reduced hepatic blood flow may delay metabolism

• Hepatic impairment — prolonged half-life; accumulation risk with infusions

• Seizure disorders — lidocaine may lower seizure threshold at toxic levels

• Respiratory compromise — CNS depression may worsen hypoventilation

• Acidosis or hypoxia — increases risk of systemic toxicity

• Mucosal application — enhanced systemic absorption; use minimal effective dose

• Children — large surface area to body weight ratio increases absorption

• Concurrent use of other local anaesthetics — additive toxicity

• Application near end-arteries (digits, penis, nose, ears) — avoid adrenaline-containing formulations

Parameter Details

Safety Category Generally considered safe (Category B equivalent); extensive obstetric experience

Preferred alternatives Lidocaine is appropriate first-line local anaesthetic in pregnancy

When to use Commonly used for epidural analgesia in labour; local infiltration for episiotomy; nerve blocks

Monitoring Fetal heart rate monitoring during epidural use; avoid repeated large doses near term; use preservative-free formulations

Parameter Details

Compatibility Compatible with breastfeeding

Drug levels in milk Low — minimal transfer after local/regional anaesthesia

Preferred alternatives Lidocaine is acceptable; no need to interrupt breastfeeding

Infant monitoring Drowsiness, feeding difficulties (rare); no routine monitoring required

Parameter Recommendation

Starting dose Lower end of dose range for all routes

Titration Slower titration for IV infusion; reduce maintenance infusion by 25–50%

Special considerations Reduced hepatic blood flow and metabolism; increased CNS sensitivity; lower albumin binding increases free drug fraction

Additional risks Enhanced risk of CNS toxicity (confusion, seizures); cardiac depression; hypotension

Monitoring ECG, blood pressure, mental status; consider serum levels if prolonged IV use

Drug Mechanism Clinical Effect Recommendation

Amiodarone Additive cardiac depression; reduced hepatic metabolism Enhanced cardiac toxicity (bradycardia, heart block) Avoid combination or reduce lidocaine dose significantly; continuous ECG monitoring

Beta-blockers (propranolol, metoprolol) Reduced hepatic blood flow; decreased lidocaine clearance Increased lidocaine levels and toxicity risk Reduce lidocaine infusion dose; monitor closely

Strong CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir) Inhibited lidocaine metabolism Elevated lidocaine levels; toxicity risk Avoid prolonged IV lidocaine or reduce dose substantially

Erythromycin, Clarithromycin CYP3A4 inhibition Increased lidocaine levels Use with caution; monitor for toxicity signs

Phenytoin Additive cardiac depression; CYP induction Enhanced cardiac toxicity with IV use; reduced efficacy with chronic phenytoin Avoid IV lidocaine in unstable patients on phenytoin

Other Class I antiarrhythmics (mexiletine, flecainide) Additive cardiac and CNS depression Enhanced toxicity Avoid concurrent use

Drug Interaction Recommendation

Rifampicin CYP3A4/CYP1A2 induction; increased lidocaine metabolism Reduced lidocaine efficacy; may need higher doses

Carbamazepine CYP3A4 induction Shortened duration of action; monitor efficacy

Cimetidine CYP inhibition (high doses) Prolonged lidocaine half-life; monitor for toxicity with IV use

Diuretics (furosemide, thiazides) Electrolyte imbalance (hypokalaemia) Hypokalaemia may exacerbate arrhythmogenic potential; monitor electrolytes

Adrenaline (in combination formulations) Prolongs local anaesthetic action; systemic absorption Avoid in end-artery regions; monitor for systemic catecholamine effects

Bupivacaine, Ropivacaine (other local anaesthetics) Additive toxicity Calculate combined doses; do not exceed total maximum dose

Local/Regional Use:

• Injection site pain and bruising

• Local tissue irritation (topical use)

• Transient numbness beyond target area

Systemic (Dose-Related CNS Effects — Early Toxicity Signs):

• Dizziness, lightheadedness

• Drowsiness

• Circumoral and tongue numbness

• Metallic taste

• Tinnitus

• Visual disturbances

Cardiovascular:

• Hypotension (particularly with epidural use)

• Bradycardia

CNS Toxicity (Progressive):

• Seizures — discontinue immediately; manage with benzodiazepines; ensure airway protection

• CNS depression — progressing to respiratory arrest

Cardiovascular Toxicity:

• Cardiac arrhythmias — bradycardia, heart block, ventricular arrhythmias

• Cardiovascular collapse — particularly with inadvertent intravascular injection

• Cardiac arrest — requires immediate ACLS with lipid emulsion therapy

Other Serious Effects:

• Methemoglobinaemia — rare; more common with prilocaine but reported with lidocaine; cyanosis unresponsive to oxygen

• Anaphylaxis — rare with amide-type anaesthetics; more common with ester-type

• Allergic contact dermatitis — with topical formulations

⚠️ Resuscitation equipment and lipid emulsion (Intralipid 20%) must be immediately available when using regional anaesthesia techniques.

Phase Parameters

Baseline Blood pressure, ECG (if IV use); hepatic function (if prolonged IV infusion planned); neurological status

During procedure Continuous verbal contact (awake patient); vital signs; early toxicity symptoms (perioral numbness, tinnitus, metallic taste)

IV antiarrhythmic use Continuous ECG; blood pressure every 5 minutes during bolus; CNS status

Prolonged IV infusion (>24 hours) Serum lidocaine levels (therapeutic: 1.5–5 mcg/mL; toxic: >6 mcg/mL); hepatic function

Epidural/Spinal Blood pressure; sensory/motor block level; fetal heart rate (obstetric use)

Plain Lidocaine Injection:

• Xylocard® (AstraZeneca)

• Lignox® (Neon)

• Loxicard® (Zydus)

• Lignocaine Injection (multiple generics)

Lidocaine with Adrenaline:

• Lignox-A® (Neon)

• Xylocaine with Adrenaline® (AstraZeneca)

Topical Formulations:

• Xylocaine Jelly® (AstraZeneca)

• Lox 2% Gel® (Neon)

• Lignocaine Gel (generics)

• LOX 10% Spray® (Neon)

• Xylocaine 10% Spray® (AstraZeneca)

Transdermal Patch (Limited Availability):

• Lidoderm® (limited import)

Note: Included in NLEM 2022 under local anaesthetics; may be available free/subsidised in government facilities.

• Preservative-free mandatory: Always use preservative-free formulations for spinal, epidural, and intrathecal administration — preservatives are neurotoxic

• Early toxicity recognition: Circumoral numbness, metallic taste, and tinnitus are early warning signs of systemic toxicity — stop injection immediately and monitor

• Adrenaline restrictions: Avoid adrenaline-containing formulations in end-artery regions (digits, penis, nose tip, ear lobes) — risk of ischaemic necrosis

• Lipid rescue: Intralipid 20% (1.5 mL/kg bolus, followed by 0.25 mL/kg/min infusion) is life-saving for local anaesthetic systemic toxicity (LAST) — should be immediately available for regional anaesthesia

• Elderly and hepatic impairment: Reduce IV infusion dose by 50% — accumulation occurs rapidly due to reduced hepatic clearance

• Antiarrhythmic hierarchy: Lidocaine is no longer first-line for VT/VF — amiodarone preferred in most ACLS scenarios; lidocaine remains useful when amiodarone unavailable or contraindicated

lidocaine; lignocaine; local anaesthetic; amide anaesthetic; antiarrhythmic; ACLS; topical anaesthesia; epidural; spinal; regional anaesthesia; NLEM India; paediatric; pregnancy-safe; hepatic metabolism; Schedule H

RxIndia v1.0 — 09 Apr 2025

• CDSCO approved formulations list

• NLEM 2022

• Indian Pharmacopoeia 2018

• API Textbook of Medicine — Cardiac Arrhythmias

• AIIMS Anaesthesia Protocol Manual

• ICMR/AIIMS Emergency Medicine Protocols

• Harrison's Principles of Internal Medicine

• Goodman & Gilman's The Pharmacological Basis of Therapeutics

• IAP Guidelines (paediatric dosing)

• WHO Essential Medicines List (supportive)